EP3838887A4 - Sel de 2-(1)-acyloxypentyl) acide benzoïque formé par un acide aminé basique ou aminoguanidine, son procédé de préparation et ses applications - Google Patents

Sel de 2-(1)-acyloxypentyl) acide benzoïque formé par un acide aminé basique ou aminoguanidine, son procédé de préparation et ses applications Download PDF

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Publication number
EP3838887A4
EP3838887A4 EP18941434.5A EP18941434A EP3838887A4 EP 3838887 A4 EP3838887 A4 EP 3838887A4 EP 18941434 A EP18941434 A EP 18941434A EP 3838887 A4 EP3838887 A4 EP 3838887A4
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EP
European Patent Office
Prior art keywords
acyloxypentyl
aminoguanidine
preparation
basic amino
method therefor
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP18941434.5A
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German (de)
English (en)
Other versions
EP3838887A1 (fr
EP3838887B1 (fr
Inventor
Yihua Zhang
Zhangjian HUANG
Jianbing Wu
Jiayi Zhu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Jiangsu Kanion Pharmaceutical Co Ltd
Original Assignee
China Pharmaceutical University
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Publication of EP3838887A4 publication Critical patent/EP3838887A4/fr
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/02—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
    • C07C69/12—Acetic acid esters
    • C07C69/14—Acetic acid esters of monohydroxylic compounds
    • C07C69/145—Acetic acid esters of monohydroxylic compounds of unsaturated alcohols
    • C07C69/157—Acetic acid esters of monohydroxylic compounds of unsaturated alcohols containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/76—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • C07C69/78—Benzoic acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/26—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing carboxyl groups by reaction with HCN, or a salt thereof, and amines, or from aminonitriles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/26—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C277/00—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C277/08—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups of substituted guanidines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/02—Guanidine; Salts, complexes or addition compounds thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/12—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/14—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C281/00—Derivatives of carbonic acid containing functional groups covered by groups C07C269/00 - C07C279/00 in which at least one nitrogen atom of these functional groups is further bound to another nitrogen atom not being part of a nitro or nitroso group
    • C07C281/16—Compounds containing any of the groups, e.g. aminoguanidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/08—Preparation of carboxylic acid esters by reacting carboxylic acids or symmetrical anhydrides with the hydroxy or O-metal group of organic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/02—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
    • C07C69/22—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety
    • C07C69/24—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with monohydroxylic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EP18941434.5A 2018-11-28 2018-12-03 Sel de 2-(1)-acyloxypentyl) acide benzoïque formé par un acide aminé basique ou aminoguanidine, son procédé de préparation et ses applications Active EP3838887B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201811440339.8A CN109678715B (zh) 2018-11-28 2018-11-28 2-(1-酰氧正戊基)苯甲酸与碱性氨基酸或氨基胍形成的盐、其制备方法及用途
PCT/CN2018/118879 WO2020107500A1 (fr) 2018-11-28 2018-12-03 Sel de 2-(1)-acyloxypentyl) acide benzoïque formé par un acide aminé basique ou aminoguanidine, son procédé de préparation et ses applications

Publications (3)

Publication Number Publication Date
EP3838887A1 EP3838887A1 (fr) 2021-06-23
EP3838887A4 true EP3838887A4 (fr) 2022-03-30
EP3838887B1 EP3838887B1 (fr) 2022-10-05

Family

ID=66185967

Family Applications (1)

Application Number Title Priority Date Filing Date
EP18941434.5A Active EP3838887B1 (fr) 2018-11-28 2018-12-03 Sel de 2-(1)-acyloxypentyl) acide benzoïque formé par un acide aminé basique ou aminoguanidine, son procédé de préparation et ses applications

Country Status (9)

Country Link
US (1) US11814352B2 (fr)
EP (1) EP3838887B1 (fr)
JP (1) JP7264999B2 (fr)
KR (1) KR102563378B1 (fr)
CN (1) CN109678715B (fr)
DK (1) DK3838887T3 (fr)
ES (1) ES2929539T3 (fr)
MY (1) MY194645A (fr)
WO (1) WO2020107500A1 (fr)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111943898A (zh) * 2019-05-17 2020-11-17 浙江大学 苯联四氮唑类衍生物、制备、含其的药物组合物及其应用
CN112457265A (zh) * 2020-11-06 2021-03-09 浙江大学 四氮唑类衍生物、制备、含其的药物组合物及其应用
CN112679353B (zh) * 2020-12-26 2022-09-20 郑州大学 一种基于丁苯酞结构的前体药物或其药学上可接受的金属盐及其制备方法和应用
CN113024422B (zh) * 2021-03-12 2022-12-20 上海科州药物研发有限公司 丁苯酞开环化合物、药物化合物以及它们的制备方法、组合物和应用
CN113105326A (zh) * 2021-03-24 2021-07-13 海南卓华制药有限公司 赖氨匹林的制备方法及应用

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1508561A1 (fr) * 2002-05-09 2005-02-23 The Institute Of Materia Medica Of Chinese Academy Of Medical Sciences 2-(g(a)-hydroxypentyl) benzoate,sa preparation et son utilisation

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9514518D0 (en) * 1995-07-15 1995-09-13 Sod Conseils Rech Applic Guanidine salt inhibitors of NO synthase and cyclooxygenase
JP2012507552A (ja) * 2008-10-29 2012-03-29 アエリエ・ファーマシューティカルズ・インコーポレーテッド プロスタグラジンのアミノ酸塩
EP4148045A1 (fr) * 2010-01-27 2023-03-15 Arena Pharmaceuticals, Inc. Composés intermédiaires pour la préparation de l'acide (r)-2-(7-(4-cyclopentyl-3-(trifluorométhyl)benzyloxy)-1,2,3,4-tétrahydrocyclopenta[b]indol-3-yl) acétique et de ses sels
EA032779B1 (ru) * 2014-03-06 2019-07-31 ПиТиСи ТЕРАПЬЮТИКС, ИНК. Фармацевтические композиции и соли 1,2,4-оксадиазолбензойной кислоты
SI3310760T1 (sl) * 2015-06-22 2023-02-28 Arena Pharmaceuticals, Inc. Kristalinična L-argininska sol (R)-2-(7-(4-ciklopentil-3-(trifluorometil)benziloksi)-1,2,3,4- tetrahidrociklo-penta(b)indol-3-il)ocetne kisline za uporabo pri motnjah, povezanih z receptorjem S1P1

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1508561A1 (fr) * 2002-05-09 2005-02-23 The Institute Of Materia Medica Of Chinese Academy Of Medical Sciences 2-(g(a)-hydroxypentyl) benzoate,sa preparation et son utilisation

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SHENG XIAO ET AL: "Novel hybrids of 3-n-butylphthalide and edaravone: Design, synthesis and evaluations as potential anti-ischemic stroke agents", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM, NL, vol. 25, no. 17, 3 July 2015 (2015-07-03), pages 3535 - 3540, XP029249470, ISSN: 0960-894X, DOI: 10.1016/J.BMCL.2015.06.090 *

Also Published As

Publication number Publication date
KR102563378B1 (ko) 2023-08-07
CN109678715B (zh) 2019-11-12
MY194645A (en) 2022-12-09
EP3838887A1 (fr) 2021-06-23
CN109678715A (zh) 2019-04-26
ES2929539T3 (es) 2022-11-30
WO2020107500A1 (fr) 2020-06-04
US11814352B2 (en) 2023-11-14
JP7264999B2 (ja) 2023-04-25
KR20210097100A (ko) 2021-08-06
US20220024848A1 (en) 2022-01-27
JP2022503890A (ja) 2022-01-12
EP3838887B1 (fr) 2022-10-05
DK3838887T3 (da) 2022-12-05

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Inventor name: ZHANG, YIHUA

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